Abstract

An efficient and practical method for the synthesis of C5-brominated 8-aminoquinoline amides via a copper-promoted selective bromination of 8-aminoquinoline amides with alkyl bromides was developed. The reaction proceeds smoothly in dimethyl sulfoxide (DMSO) under air, employing activated and unactivated alkyl bromides as the halogenation reagents without additional external oxidants. This method features outstanding site selectivity, broad substrate scope, and excellent yields.

Beilstein J. Org. Chem. 2024, 20, 155–161. doi:10.3762/bjoc.20.14

中文翻译：

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铜促进 8-氨基喹啉酰胺与烷基溴的 C5 选择性溴化

摘要

开发了一种通过铜促进 8-氨基喹啉酰胺与烷基溴选择性溴化合成 C5-溴化 8-氨基喹啉酰胺的有效且实用的方法。该反应在空气下的二甲基亚砜（DMSO）中顺利进行，采用活化和未活化的烷基溴作为卤化试剂，无需额外的外部氧化剂。该方法具有出色的位点选择性、广泛的底物范围和优异的产率。

贝尔斯坦 J. 组织。化学。 2024, 20, 155–161。doi:10.3762/bjoc.20.14